1. Field of the Invention
This invention relates to new anthracycline derivatives, to methods for their use as antimicrobial and antitumor agents, to pharmaceutical compositions containing them and to synthetic methods and intermediates for the preparation of said new derivatives.
2. Description of the Prior Art
Daunomycin (see U.S. Pat. No. 3,616,242) and adriamycin (see U.S. Pat. No. 3,590,028) obtained from fermentation broths of microorganisms of the genus Actinomyces are known as anthracycline-type antibiotics. These compounds have a broad antitumor spectrum against experimental tumors and are widely used clinically as chemotherapeutic antitumor agents.
Despite the usefulness of daunomycin and adriamycin, there is still a need for new anthracycline derivatives which will have greater antitumor activity and/or reduced toxicities. To satisfy this need, attempts have been made to provide anthracycline derivatives by fermentation, biotransformation and both semisynthetic and total synthetic processes. Illustrative of these attempts are the methods disclosed by F. Arcamone in Topics in Antibiotic Chemistry 2:102-279 (1978) and in U.S. Pat. No. 3,988,315 (aclacinomycins A and B).
U.S. Pat. No. 4,247,545 discloses the preparation of 11-deoxy derivatives of daunomycin and adriamycin (as well as their respective aglycones) by fermentation of Streptomyces peucetius var. caesius (ATCC 31366).